Ready to use LET formulations

Abstract

Disclosed herein is a pharmaceutical formulation comprising lidocaine, epinephrine, and tetracaine. Also disclosed herein is a process for preparing the pharmaceutical formulation comprising lidocaine, epinephrine, and tetracaine, as well as methods for using the pharmaceutical formulation.

The invention claimed is: 
     
       1. A ready-to-use pharmaceutical formulation, consisting of:
 a) lidocaine hydrochloride in an amount of 40 mg/mL; 
 b) epinephrine hydrochloride in an amount of 0.61 mg/mL; 
 c) tetracaine hydrochloride in an amount of 5 mg/mL; 
 d) propylene glycol in an amount of 10 mg/mL; 
 e) sodium metabisulfite in an amount of 0.265 mg/mL; 
 f) a disodium salt of ethylenediaminetetraacetic acid dihydrate (Na 2 EDTA DH) in an amount of 0.2 mg/mL; 
 g) methylparaben in an amount of 1.8 mg/mL; 
 h) hydroxyethylcellulose in an amount of 0 mg/mL, 17.6 mg/mL, or 35.2 ma/mL; and 
 i) a sufficient amount of sterile water for injection; 
 wherein the ready-to-use pharmaceutical formulation has a pH of from 3.6 to 3.9; and 
 wherein the ready-to-use pharmaceutical formulation has epinephrine hydrochloride content of 90% to 115% of the epinephrine hydrochloride content of 0.61 mg/mL after storage at a temperature ranging from 22° C. to 25° C. for 380 days. 
 
     
     
       2. A method for providing procedural analgesia to a patient in need thereof, which comprises topically administering an effective amount of the ready-to-use pharmaceutical formulation of  claim 1  to the patient in need of analgesia. 
     
     
       3. A process for preparing the ready-to-use pharmaceutical formulation of  claim 1 , which comprises:
 a) dissolving methylparaben in propylene glycol to obtain a preservative solution; 
 b) dissolving the preservative solution in water for injection to obtain a preserved water solution; 
 c) dissolving in the preserved water solution: (i) the lidocaine hydrochloride; (ii) the tetracaine hydrochloride; (iii) the sodium metabisulfite; and (iv) the Na 2 EDTA DH; 
 d) optionally, adjusting the pH of the step c) solution to a pH of from 3.6 to 3.9; 
 e) dissolving the epinephrine hydrochloride in the step c) solution or the step d) solution; 
 f) optionally, adjusting the pH of the step e) solution to a pH of from 3.6 to 3.9; 
 g) filtering the solution of step e) or the solution of step f) using a 0.2 micron polyethersulfone filter; and 
 h) optionally adding the hydroxyethylcellulose to the step g) solution. 
 
     
     
       4. The ready-to-use pharmaceutical formulation of  claim 1 , wherein the pharmaceutical formulation contains 0 mg/mL of hydroxyethylcellulose. 
     
     
       5. The ready-to-use pharmaceutical formulation of  claim 1 , wherein the hydroxyethylcellulose is present in an amount of 17.6 mg/mL. 
     
     
       6. The ready-to-use pharmaceutical formulation of  claim 1 , wherein hydroxyethylcellulose is present in an amount of about 35.2 mg/mL. 
     
     
       7. The ready-to-use pharmaceutical formulation of  claim 1 , wherein the pharmaceutical formulation has a pH of from 3.6 to 3.8. 
     
     
       8. The ready-to-use pharmaceutical formulation of  claim 1 , wherein the formulation is contained in an amber-colored syringe.